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Biomedicines
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Drug Resistance and Novel Targets for Cancer Therapy—Third Edition
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Drug Resistance and Novel Targets for Cancer Therapy—Third Edition

A special issue of Biomedicines (ISSN 2227-9059). This special issue belongs to the section "Cancer Biology and Oncology".

Deadline for manuscript submissions: 28 February 2026 | Viewed by 209

Special Issue Editors

Dr. Bruno Kaufmann Robbs

E-Mail Website
Guest Editor
Instituto de Saúde de Nova Friburgo, Universidade Federal Fluminense, Nova Friburgo, Brazil
Interests: natural product; cancer drugs; biological activity assays; chemotherapeutic; molecular targets
Special Issues, Collections and Topics in MDPI journals
Dr. Fernando de Carvalho da Silva

E-Mail Website
Guest Editor
Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Niterói 24020-141, RJ, Brazil
Interests: organic synthesis; medicinal chemistry; naphthoquinones; triazoles
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Drug resistance is a complex phenomenon resulting from one or more mechanisms that render cells resistant to anticancer drugs. The molecular hallmarks of cancer and therapeutics against drug resistance mechanisms represent the leading targets in cancer treatment. Molecular-targeted therapy is attracting growing attraction due to it being specific to cancer and able to spare normal cells. Despite this, drug resistance still represents a major obstacle limiting sustained clinical benefits, not only in targeted cancer therapies but also in conventional chemotherapy. Notably, while some cancer patients do not respond to anticancer drugs due to primary resistance, even responders might eventually relapse following acquired resistance.

In this context, we are launching a new Special Issue encompassing the two major molecular pathways in cancer treatment: the determination of new cancer-related molecular targets and the development of drugs that block them and drugs designed to prevent resistance to treatment. We invite innovative research papers and review articles discussing new molecular targets or anticancer drugs. We encourage articles related to, but not restricted to, apoptosis induction, proliferative signaling, migration, angiogenesis, metastasis, immune checkpoints, tumor vaccine-related targets, chimeric antigen receptor T-cells, or possible drug resistance mechanisms. This Special Issue will address novel molecular targets, drugs designed to attack them, and possible resistance mechanisms that could be targeted to enable more durable and effective responses in cancer therapy.

Dr. Bruno Kaufmann Robbs
Dr. Fernando de Carvalho da Silva
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 250 words) can be sent to the Editorial Office for assessment.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Biomedicines is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2600 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • cancer
  • drug resistance
  • targeted therapy
  • conventional chemotherapy
  • natural products
  • molecular targets
  • cancer hallmarks
  • therapeutic agents

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Published Papers (1 paper)

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Research

26 pages, 5062 KB  
Article
Reversing the Irreversible: miRNA-Targeting Mesyl Phosphoramidate Oligonucleotides Restore Sensitivity to Cisplatin and Doxorubicin of KB-8-5 Epidermoid Carcinoma Cells
by Svetlana Miroshnichenko, Rabia Demirel, Arseny Moralev, Olga Almieva, Andrey Markov, Ekaterina Burakova, Dmitry Stetsenko, Mikhail Maslov, Valentin Vlassov and Marina Zenkova
Biomedicines 2025, 13(12), 3118; https://doi.org/10.3390/biomedicines13123118 - 18 Dec 2025
Abstract
Background: Chemotherapy remains one of the main approaches for treating malignant tumors, but repeated exposure to cytostatics leads to multidrug resistance (MDR), increasing tumor aggressiveness and reducing therapeutic efficacy. Identifying adjuvant agents that restore tumor sensitivity to drugs while minimizing toxicity is a [...] Read more.
Background: Chemotherapy remains one of the main approaches for treating malignant tumors, but repeated exposure to cytostatics leads to multidrug resistance (MDR), increasing tumor aggressiveness and reducing therapeutic efficacy. Identifying adjuvant agents that restore tumor sensitivity to drugs while minimizing toxicity is a cornerstone challenge today. This study aimed to investigate the potential of mesyl phosphoramidate antisense oligonucleotides (µ-ASOs) targeting miR-17, miR-21, and miR-155 as agents for enhancing the efficacy of cisplatin (Cis) and doxorubicin (Dox) in MDR-positive human epidermoid carcinoma KB-8-5 cells. Methods: Optimal regimens for the simultaneous application of µ-ASOs and Dox or Cis in KB-8-5 cells, including a concentration-dependent analysis and the type of compound interaction in combinations (synergy/additivity/antagonism), were studied using the MTT assay. Antiproliferative effects of the combinations were assessed using the real-time cell monitoring xCELLigence system. The potential molecular mechanism underlying KB-8-5 cell sensitization to cytostatics was investigated using RT-PCR and Western blot hybridization, supported by bioinformatic reconstruction of the gene network. Results: The most effective combinations including µ-ASOs targeting miR-21 and miR-17 together with Cis or Dox demonstrated additive to moderately synergistic effects on KB-8-5 cell viability (HSA synergy score = 4.8–8.7). The co-application of µ-ASOs allowed a 5- to 20-fold reduction in the dose of cytostatics, while maintaining a strong antiproliferative effect of 70–95%. Sensitization of KB-8-5 cells to Cis or Dox following µ-ASO treatment was mediated by a 1.5- to 3-fold decrease in the levels of the well-known MDR marker ABCB1 as well as the newly identified MDR-associated targets ZYX, TUBA4A, and SEH1L. Conclusions: miRNA-targeted mesyl phosphoramidate oligonucleotides are effective tools for overcoming resistance to the clinically approved chemotherapeutics cisplatin and doxorubicin. The relationship between miR-21, miR-17, and miR-155 and the novel MDR markers such as SEH1L, TUBA4A, and ZYX was revealed, thereby expanding the current understanding of the molecular mechanisms underlying tumor cell resistance to chemotherapy. Full article
(This article belongs to the Special Issue Drug Resistance and Novel Targets for Cancer Therapy—Third Edition)
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